Berti F, Rossoni G, Braquet P
Department of Pharmacology Chemotherapy and Medical Toxicology, University of Milan, Italy.
Agents Actions. 1990 Jun;30(3-4):301-6. doi: 10.1007/BF01966291.
The ability of a specific PAF-receptor antagonist, BN-52021, to control the release of mediators of anaphylaxis from actively sensitized (ovalbumin) guinea-pig has been investigated "in vitro". BN-52021 perfused through the kidney at different molar concentrations (1 x 10(-4)-1 x 10(-5)-1 x 10(-6] prior to antigen challenge neither modified the basal values of perfusion pressure nor stimulated mediator release from the organ. On the contrary, the compound antagonized in a concentration dependent way both vasoconstriction of the renal vessels and the increase in the perfusate of histamine, TXB2 and SRS-A due to antigenic shock. The antagonistic activity of BN-52021 was very consistent at 1 x 10(-4) M at which concentration the immunological release of histamine and TXB2 was reduced by 75%. The beneficial effect of BN-52021 in experimental anaphylaxis of the kidney may have some therapeutic implications principally in those pathological conditions where an abnormal increase of renal histamine and other mediators may compromise the haemodynamic function of this organ.
一种特定的血小板活化因子(PAF)受体拮抗剂BN - 52021在体外对主动致敏(卵清蛋白)豚鼠过敏反应介质释放的控制能力已被研究。在抗原攻击前,以不同摩尔浓度(1×10⁻⁴ - 1×10⁻⁵ - 1×10⁻⁶)通过肾脏灌注BN - 52021,既未改变灌注压的基础值,也未刺激该器官释放介质。相反,该化合物以浓度依赖性方式拮抗肾血管的血管收缩以及由于抗原休克导致的组胺、TXB₂和慢反应物质 - A(SRS - A)灌流液增加。BN - 52021在1×10⁻⁴ M时的拮抗活性非常一致,在此浓度下,组胺和TXB₂的免疫释放减少了75%。BN - 52021在实验性肾过敏反应中的有益作用可能具有一些治疗意义,主要针对那些肾组胺和其他介质异常增加可能损害该器官血液动力学功能的病理状况。